KR920014810A - Antibacterial agents - Google Patents

Antibacterial agents Download PDF

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Publication number
KR920014810A
KR920014810A KR1019920000198A KR920000198A KR920014810A KR 920014810 A KR920014810 A KR 920014810A KR 1019920000198 A KR1019920000198 A KR 1019920000198A KR 920000198 A KR920000198 A KR 920000198A KR 920014810 A KR920014810 A KR 920014810A
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KR
South Korea
Prior art keywords
compound
alkyl
hydrogen
amino
nitrogen
Prior art date
Application number
KR1019920000198A
Other languages
Korean (ko)
Inventor
존 테르난스키 로버트
Original Assignee
리로이 휘테커
일라이 릴리 앤드 캄파니
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by 리로이 휘테커, 일라이 릴리 앤드 캄파니 filed Critical 리로이 휘테커
Publication of KR920014810A publication Critical patent/KR920014810A/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D463/00—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring
    • C07D463/10—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2
    • C07D463/14—Heterocyclic compounds containing 1-azabicyclo [4.2.0] octane ring systems, i.e. compounds containing a ring system of the formula:, e.g. carbacephalosporins; Such ring systems being further condensed, e.g. 2,3-condensed with an oxygen-, nitrogen- or sulfur-containing hetero ring with a carbon atom having three bonds to hetero atoms with at the most one bond to halogen, e.g. an ester or nitrile radical, directly attached in position 2 with hetero atoms directly attached in position 7
    • C07D463/16—Nitrogen atoms
    • C07D463/18—Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof
    • C07D463/20—Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof with the acylating radicals further substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D463/22—Nitrogen atoms further acylated by radicals derived from carboxylic acids or by nitrogen or sulfur analogues thereof with the acylating radicals further substituted by hetero atoms or by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen further substituted by nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

내용 없음No content

Description

항균제Antibacterial agents

본 내용은 요부공개 건이므로 전문내용을 수록하지 않았음Since this is an open matter, no full text was included.

Claims (12)

하기 일반식(1)의 화합물 또는 그의 약학적으로 허용 가능한 염 :A compound of formula (1) or a pharmaceutically acceptable salt thereof: 상기 식에서 R은 수소, C1-C6알킬, C2-C6알케닐, C2-C|6알키닐, C3-C6사이클로알킬 또는 C1-C6할로알킬이고, A 및 A'는 독립적으로 수소, C1-C6알킬, 니트로, 아미노, 질소 및 황중에서 선택된 1,2또는 3개의 헤테로원자를 함유하는 5 내지 6원의 유기 헤테로사이클, C1-C6알콕시 또는 페닐이거나, 또는 A 및 A'는 함께 일반식Wherein R is hydrogen, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C | 6 alkynyl, C 3 -C 6 cycloalkyl or C 1 -C 6 haloalkyl, A and A ′ are independently 1,2, selected from hydrogen, C 1 -C 6 alkyl, nitro, amino, nitrogen and sulfur; A 5-6 membered organic heterocycle containing 3 heteroatoms, C 1 -C 6 alkoxy or phenyl, or A and A ′ together are (여기에서, X는 수소, 할로, C1-C6알킬, C1-C6알콕시, C1-C6알콕시카보닐, 아미노, 니트로 또는 카복시이고, Y는 질소 또는 탄소이다)의 그룹을 형성한다.Wherein X is hydrogen, halo, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxycarbonyl, amino, nitro or carboxy and Y is nitrogen or carbon Form. 제1항에 있어서, R이 C1-C6알킬 또는 C1-C6할로알킬인 화합물.The compound of claim 1, wherein R is C 1 -C 6 alkyl or C 1 -C 6 haloalkyl. 제2항에 있어서, R이 메틸 또는 플루오로 -C1-C6알킬인 화합물.The compound of claim 2, wherein R is methyl or fluoro-C 1 -C 6 alkyl. 제3항에 있어서, R이 2-플루오로에트-1-일인 화합물.The compound of claim 3, wherein R is 2-fluoroeth-1-yl. 제1항에 있어서, A 및 A'가 일반식A compound according to claim 1, wherein A and A ' 의 그룹을 형성하는 화합물.Compounds that form a group. 제5항에 있어서, Y가 질소인 화합물.The compound of claim 5, wherein Y is nitrogen. 제6항에 있어서, A 및 A' 가 구조식7. A compound according to claim 6 wherein A and A 'are structural formulas 의 그룹을 형성하는 화합물.Compounds that form a group. 제7항에 있어서, R이 메틸 또는 2-플루오로에틸인 화합물.8. A compound according to claim 7, wherein R is methyl or 2-fluoroethyl. 하기 일반식(2)의 화합물 :Compound of the following general formula (2): 상기 식에서, R0는 아미노 또는 보호된 아미노이고, R1은 수소 또는 카복시-보호 그룹이며 A 및 A'는 독립적으로 수소, C1-C6알킬, 페닐, 니트로, 아미노, 질소 및 황중에서 선택된 1,2또는 3개의 헤테로원자를 함유하는 5 내지 6원의 유기 헤테로사이클 또는 C1-C6알콕시이거나, 또는 A 및 A'는 함께 일반식Wherein R 0 is amino or protected amino, R 1 is hydrogen or a carboxy-protecting group and A and A 'are independently selected from hydrogen, C 1 -C 6 alkyl, phenyl, nitro, amino, nitrogen and sulfur A 5-6 membered organic heterocycle or C 1 -C 6 alkoxy containing 1,2 or 3 heteroatoms, or A and A ′ together are (여기에서, X는 수소, C1-C6알킬, C1-C6알콕시, C1-C6알콕시카보닐, 아미노, 니트로, 또는 카복시이고, Y는 질소 또는 탄소이다)의 그룹을 형성한다.Wherein X is hydrogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 alkoxycarbonyl, amino, nitro, or carboxy, and Y is nitrogen or carbon do. 제9항에 있어서, A 및 A'가 함께 일반식10. A compound according to claim 9 wherein A and A 'together 의 그룹을 형성하는 화합물.Compounds that form a group. 제10항에 있어서, A 및 A'가 구조식11. A compound according to claim 10 wherein A and A 'are structural formulas 의 그룹을 형성하는 화합물.Compounds that form a group. 하나 이상의 약학적으로 허용가능한 담체, 부형제 또는 희석제와 함께 제1항 내지 제8항중 어느 한 항에 청구된 화합물을 포함하는 약학 조성물.A pharmaceutical composition comprising a compound as claimed in any one of claims 1 to 8 together with one or more pharmaceutically acceptable carriers, excipients or diluents. ※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.※ Note: The disclosure is based on the initial application.
KR1019920000198A 1991-01-18 1992-01-09 Antibacterial agents KR920014810A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US07/643,244 1991-01-18
US07/643,244 US5077287A (en) 1991-01-18 1991-01-18 3-thiazolylthio carbacephem antibacterial agents

Publications (1)

Publication Number Publication Date
KR920014810A true KR920014810A (en) 1992-08-25

Family

ID=24579974

Family Applications (1)

Application Number Title Priority Date Filing Date
KR1019920000198A KR920014810A (en) 1991-01-18 1992-01-09 Antibacterial agents

Country Status (21)

Country Link
US (1) US5077287A (en)
EP (1) EP0495585A1 (en)
JP (1) JPH04321686A (en)
KR (1) KR920014810A (en)
CN (1) CN1063284A (en)
AU (1) AU642334B2 (en)
BR (1) BR9200058A (en)
CA (1) CA2058592C (en)
CZ (1) CZ281909B6 (en)
FI (1) FI920110A (en)
HU (1) HUT60268A (en)
IE (1) IE920084A1 (en)
IL (1) IL100575A (en)
MX (1) MX9200105A (en)
MY (1) MY131300A (en)
NO (1) NO301328B1 (en)
NZ (1) NZ241250A (en)
PT (1) PT99984B (en)
RU (1) RU2107067C1 (en)
YU (1) YU2392A (en)
ZA (1) ZA9225B (en)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5272265A (en) * 1990-02-12 1993-12-21 Eli Lilly And Company 3-(substituted or unsubstituted) thiazolo-1-carba (1-dethia)cephems
US5179088A (en) * 1990-02-12 1993-01-12 Eli Lilly And Company 1-carba(dethia)cephalosporin antibiotics
IL100576A (en) * 1991-01-18 1995-11-27 Eli Lilley And Company Cephalosporin antibiotics
JP3238209B2 (en) * 1992-09-30 2001-12-10 塩野義製薬株式会社 Thiomethylthiocarbacephalosporin derivative
US5525599A (en) * 1993-07-21 1996-06-11 Eli Lilly And Company 7-substituted-amino-3-substituted-3-cephem-4-carboxylic acids
DE4333697A1 (en) * 1993-10-02 1995-04-06 Merck Patent Gmbh Process for the preparation of 3-aminopyridines from 3-nitropyridines
US5496816A (en) * 1994-03-14 1996-03-05 Merck & Co., Inc. Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment
US5688786A (en) * 1994-04-01 1997-11-18 Microcide Pharmaceuticals, Inc. β-lactam antibiotics
US5698547A (en) * 1994-04-01 1997-12-16 Microcide Pharmaceuticals, Inc. Cephalosporin antibiotics
NZ284212A (en) * 1994-04-01 1997-11-24 Microcide Pharmaceuticals Inc Cephalosporin antibiotics; antibacterial medicament
US5498777A (en) * 1994-07-20 1996-03-12 Merck & Co., Inc. 3-thioheteroaryl cephalosporin compounds, compositions and methods of use
US5565445A (en) * 1995-02-22 1996-10-15 Merck & Co., Inc. 3-thioheteroaryl 1-carba-1-dethiacephalosporin compounds, compositions and methods of use
WO1996038450A1 (en) * 1995-05-31 1996-12-05 Microcide Pharmaceuticals, Inc. Cephalosporin antibiotics
MY127641A (en) * 1995-10-12 2006-12-29 Essential Therapeutics Inc Cephalosporin antibiotics
WO1998046566A1 (en) * 1997-04-17 1998-10-22 Microcide Pharmaceuticals, Inc. IMPROVED β-LACTAM ANTIBIOTICS
US6025352A (en) * 1997-09-29 2000-02-15 Microcide Pharmaceuticals, Inc. Cephalosporin antibiotics
US6030965A (en) * 1997-09-30 2000-02-29 Microcide Pharmaceuticals, Inc. Cephalosporin antibiotics
US6362009B1 (en) 1997-11-21 2002-03-26 Merck & Co., Inc. Solid phase synthesis of heterocycles
ATE449775T1 (en) * 2003-04-30 2009-12-15 Trine Pharmaceuticals Inc CARBACEPHEM BETA-LACTAM ANTIBIOTICS
US20080146535A1 (en) * 2003-04-30 2008-06-19 Tomasz Glinka Compositions comprising carbacephem beta-lactam antibiotics and beta-lactamase inhibitors
KR20100093532A (en) * 2007-10-25 2010-08-25 아카오젠, 인코포레이티드 CARBACEPHEM β-LACTAM ANTIBIOTICS
WO2010030810A1 (en) * 2008-09-10 2010-03-18 Achaogen, Inc. Carbacephem beta-lactam antibiotics
WO2010123997A1 (en) * 2009-04-22 2010-10-28 Achaogen, Inc. Carbacephem beta-lactam antibiotics
WO2011103441A1 (en) 2010-02-18 2011-08-25 Schering Corporation Substituted pyridine and pyrimidine derivatives and their use in treating viral infections

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA766941B (en) * 1975-11-21 1978-06-28 Merck & Co Inc 3-(substituted thio)cephalosporins,derivatives and nuclear analogues thereof
JPS6058920B2 (en) * 1978-12-26 1985-12-23 協和醗酵工業株式会社 Cephalosporin analogs
JPS60174787A (en) * 1984-02-21 1985-09-09 Kyowa Hakko Kogyo Co Ltd 3-position-substituted carbacephem compound
JPH0653739B2 (en) * 1984-11-15 1994-07-20 協和醗酵工業株式会社 3-position substituted carbacephem compound
US4885291A (en) * 1988-01-14 1989-12-05 Eli Lilly And Company 1-carba(dethia)-3-cephem derivatives
IL100576A (en) * 1991-01-18 1995-11-27 Eli Lilley And Company Cephalosporin antibiotics

Also Published As

Publication number Publication date
HUT60268A (en) 1992-08-28
RU2107067C1 (en) 1998-03-20
FI920110A0 (en) 1992-01-10
YU2392A (en) 1994-12-28
MX9200105A (en) 1992-07-01
MY131300A (en) 2007-08-30
FI920110A (en) 1992-07-19
CN1063284A (en) 1992-08-05
HU9200081D0 (en) 1992-03-30
PT99984A (en) 1993-01-29
IL100575A0 (en) 1992-09-06
NZ241250A (en) 1993-02-25
IE920084A1 (en) 1992-07-29
IL100575A (en) 1996-11-14
CZ281909B6 (en) 1997-03-12
EP0495585A1 (en) 1992-07-22
CA2058592A1 (en) 1992-07-19
NO920103D0 (en) 1992-01-08
PT99984B (en) 1999-06-30
US5077287A (en) 1991-12-31
AU1013592A (en) 1992-07-23
CS1192A3 (en) 1992-08-12
NO301328B1 (en) 1997-10-13
JPH04321686A (en) 1992-11-11
BR9200058A (en) 1992-09-08
ZA9225B (en) 1993-07-02
CA2058592C (en) 2001-12-25
NO920103L (en) 1992-07-20
AU642334B2 (en) 1993-10-14

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